Abstract: The invention provides a method and a composition for enhancing the dissolution and bioavailable properties of propofol (2, 6 diisopropyl phenol) for use as an intravenously administered anesthetic in mammals. The method produces a self-microemulsifyable emulsion base composition that is utilized in the production of a water-based microemulsion preparation. In a preferred two (2) component base composition, the base composition consists of: a surfactant, containing polyethylene glycol; and liquid propofol. The microemulsion is prepared by mixing the base composition with a carrier liquid, which results in the formation of a microemulsion containing concentrations of propofol of up to about 4% by weight of propofol to the volume of the microemulsion. In a four (4) component base composition, the base composition consists of: a surfactant, containing polyethylene glycol; liquid propofol; a water-immiscible solvent; and ethanol.

Abstract: The presently disclosed subject matter relates to pharmaceutical compositions comprising dexmedetomidine or a pharmaceutically acceptable salt thereof wherein the composition is formulated as a liquid for parenteral administration to a subject, and wherein the composition is disposed within a sealed container as a premixture. The pharmaceutical compositions can be used, for example, in perioperative care of a patient or for sedation.

Abstract: The presently disclosed subject matter relates to pharmaceutical compositions comprising dexmedetomidine or a pharmaceutically acceptable salt thereof wherein the composition is formulated as a liquid for parenteral administration to a subject, and wherein the composition is disposed within a sealed container as a premixture. The pharmaceutical compositions can be used, for example, in perioperative care of a patient or for sedation.

Abstract: The presently disclosed subject matter relates to pharmaceutical compositions comprising dexmedetomidine or a pharmaceutically acceptable salt thereof wherein the composition is formulated as a liquid for parenteral administration to a subject, and wherein the composition is disposed within a sealed container as a premixture. The pharmaceutical compositions can be used, for example, in perioperative care of a patient or for sedation.

Abstract: The invention provides a method and a composition for enhancing the dissolution and bioavailable properties of propofol (2, 6 diisopropyl phenol) for use as an intravenously administered anesthetic in mammals. The method produces a self-microemulsifiable emulsion base composition that is utilized in the production of a water-based microemulsion preparation. In a preferred two (2) component base composition, the base composition consists of: a surfactant, containing polyethylene glycol; and liquid propofol. The microemulsion is prepared by mixing the base composition with a carrier liquid, which results in the formation of a microemulsion containing concentrations of propofol of up to about 4% by weight of propofol to the volume of the microemulsion. In a four (4) component base composition, the base composition consists of: a surfactant, containing polyethylene glycol; liquid propofol; a water-immiscible solvent; and ethanol.

Abstract: The presently disclosed subject matter relates to pharmaceutical compositions comprising dexmedetomidine or a pharmaceutically acceptable salt thereof wherein the composition is formulated as a liquid for parenteral administration to a subject, and wherein the composition is disposed within a sealed container as a premixture. The pharmaceutical compositions can be used, for example, in perioperative care of a patient or for sedation.

Abstract: The present invention provides a substantially clear gel designed to reduce itching discomfort when applied to the vulvar tissue. The gel includes at least one anesthetic, protectant, emulsifier, and pH modifier, such as a base. The gel has a pH adapted to vulvar use and may be applied to the vulvar tissues.

Abstract: The presently disclosed subject matter relates to pharmaceutical compositions comprising dexmedetomidine or a pharmaceutically acceptable salt thereof wherein the composition is formulated as a liquid for parenteral administration to a subject, and wherein the composition is disposed within a sealed container as a premixture. The pharmaceutical compositions can be used, for example, in perioperative care of a patient or for sedation.

Abstract: This invention relates to a patch for the expulsion of insect poison from the skin after stings from membranous insects (Hymenoptera). The patch is characterized in comprising a poison-aspirating matrix comprising an expulsion agent as well as a swell layer, which swells after the addition of a liquid through a hole on the top of the patch and thus adds a light pressure to the poison-aspirating matrix towards the skin, whereby a local and relieving effect is achieved. In one embodiment, the matrix further comprises a local anesthetic. The expulsion agent is e.g. a carbohydrate. The swell layer consists e.g. of a silica gel.

Abstract: The present invention provides methods of using halogenated volatile compounds, e.g., halogenated ether, for treating a neurological disorder, e.g., Parkinson's disease.

Abstract: The invention provides pharmaceutical compositions comprising a phenylacetic acid ester compound useful for inducing or maintaining general anesthesia or sedation in mammals, methods for preparing such compositions, and methods for inducing or maintaining anesthesia or sedation using such compositions.

Abstract: The present invention has as objective the stabilization of a fluoroether compound against degradation by acid substances. The stabilizers proposed are selected among propylene glycol, polyethylene glycol, hexylene glycol, 1,3-butylene glycol and a saturated cyclic alcohol preferably menthol and are used for preparing stable pharmaceutical compositions of a fluoroether compound. Method for stabilizing a fluoroether compound and use of stabilizers agents for precluding the degradation of a fluoroether are also described.

Abstract: The invention provides pharmaceutical compositions comprising a phenylacetic acid ester compound useful for inducing or maintaining general anesthesia or sedation in mammals, methods for preparing such compositions, and methods for inducing or maintaining anesthesia or sedation using such compositions.

Abstract: A high throughput neurophysiological assay for identifying anti-psychotic compounds is disclosed. In particular, a high throughput neurophysiological assay using information obtained from injecting a neural activity blocker, such as tetrodotoxin (TTX), into one hippocampus persistently coactivated pyramidal cells in the uninjected hippocampus that initially discharged independently. In accord with the definition of cognitive disorganization, pyramidal cell firing rates only changed for 15 min and did not accompany the coactivation. The disclosed assay uses the TTX-induced coactivity of hippocampal pyramidal cell discharge to identify compounds that may prevent or attenuate the changes in the hippocampal pyramidal cell discharge observed when a neural activity blocker is administered. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that have anti-psychotic properties.

Abstract: Disclosed herein is a preparation for topically delivering and localizing therapeutic agents, comprising: a vasoconstrictor for retarding vascular dispersion of a therapeutic agent; and a penetration enhancer for facilitating penetration of the vasoconstrictor and the therapeutic agent through a patient's skin. Further disclosed is an associated method of topically delivering and localizing therapeutic agents, comprising the steps of: using a vasoconstrictor for retarding vascular dispersion of a therapeutic agent; in combination with using a penetration enhancer for facilitating penetration of the vasoconstrictor and the therapeutic agent through a patient's skin. Also disclosed are various courses of treatment which comprise applying the various disclosed combinations of agents to the patient's skin.

Abstract: In a first aspect, the present invention relates to the use of xenon in the preparation of a medicament for providing analgesia in a newborn subject and/or a fetal subject. In a second aspect, the invention relates to a method of providing analgesia in a newborn subject, the method comprising administering to the subject a therapeutically effective amount of xenon. In a third aspect, the invention relates to a method of providing analgesia in a fetal subject, the method comprising administering to the mother of the fetal subject a therapeutically effective amount of xenon for both the mother and fetal subject.

Abstract: A medicament for therapeutic and/or prophylactic treatment of neuropathic pain, which comprises a compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient: wherein R1 represents a hydrogen atom or a hydroxyl group; R2 represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms; R3 represents a phenyl group which may have 1 to 3 atoms or substituents selected from the group consisting of a halogen atom, a hydroxyl group, an alkyl group having 1 to 3 carbon atoms, and an alkoxyl group having 1 to 3 carbon atoms, or represents —NH—R4 wherein R4 represents a phenyl group which may have 1 to 3 atoms or substituents selected from the group consisting of a halogen atom, a hydroxyl group, an alkyl group having 1 to 3 carbon atoms, and an alkoxyl group having 1 to 3 carbon atoms or hydrogen atom, and n represents 0 or 1.

Abstract: The present invention relates to methods of controlling neurological deficits in patients who have undergone cardiopulmonary bypass (CPB) by administering xenon to said patients.

Abstract: Spinal anesthetics for intrathecal administration to produce spinal anesthesia are provided with use of 6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahydroisoquinolone-3-carboxylic acid or its pharmaceutically active analogues.

Abstract: The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.

Abstract: Irritation upon injection of a formulation containing propofol is reduced or substantially eliminated by administering a stable, sterile, and antimicrobial aqueous dispersion comprising a water-insoluble microdroplet matrix of mean diameter from about 50 nm to about 1000 nm consisting essentially of about 1% to about 15% of propofol, up to about 7% of a propofol-soluble diluent, and about 0.8% to about 4% of a surface stabilizing amphiphilic agent. The aqueous phase includes a pharmaceutically acceptable water-soluble polyhydroxy tonicity modifier. The propofol-containing dispersion is devoid of additional bactericidal or bacteriostatic preservative agents.

Abstract: Spinal anesthetics for intrathecal administration to produce spinal anesthesia are provided with use of 6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahydroisoquinolone-3-carboxylic acid or a pharmaceutically active analogue or its pharmaceutically active analogs.

Abstract: This invention relates to a pharmaceutical composition for oral administration comprising a carrier and, as active ingredient, an opioid (? receptor) agonist, such as fentanyl, or a salt thereof, characterized in that the composition is in the form of a fast-dispersing dosage form designed to release the active ingredient rapidly in the oral cavity. A process for preparing such a composition and the use of such a composition as an analgesic, for the treatment of chronic pain and/or breakthrough pain, as an anesthetic premedication, for the induction of anesthesia, as a sedative and/or for the treatment of anxiety are also provided.

Abstract: Irritation upon injection of a formulation containing propofol is reduced or substantially eliminated by administering a stable, sterile, and antimicrobial aqueous dispersion comprising a water-insoluble microdroplet matrix of mean diameter from about 50 nm to about 1000 nm consisting essentially of about 1% to about 15% of propofol, up to about 7% of a propofol-soluble diluent, and about 0.8% to about 4% of a surface stabilizing amphiphilic aent. The aqueous phase includes a pharmaceutically acceptable water-soluble polyhydroxy tonicity modifier. The propofol-containing dispersion is devoid of additional bactericidal or bacteriostatic preservative agents.

Abstract: Several lines of evidence have shown a role for the nitric oxide (NO)/cyclic guanosine monophosphate (cGMP) signaling pathway in the development of spinal hyperalgesia. However, the roles of effectors for cGMP are not fully understood in the processing of pain in the spinal cord. cGMP-dependent protein kinase (PKG) I? but not PKGI? was localized in the neuronal bodies and processes, and was distributed primarily in the superficial laminae of the spinal cord. Intrathecal administration of an inhibitor of PKGI?, Rp-8-[(4-Chlorophenyl)thio]-cGMPS triethylamine, produces significant antinociception. Moreover, PKGI? protein expression was dramatically increased in the lumbar spinal cord after noxious stimulation. This upregulation of PKGI? expression was completely blocked not only by a neuronal NO synthase inhibitor, and a soluble guanylate cyclase inhibitor, but also by an N-methyl-D-aspartate (NMDA) receptor antagonist, MK-801.

Abstract: Block copolymers based on poly(ortho esters) containing amine groups. These block copolymers have both hydrophilic and hydrophobic blocks. They form micelles in aqueous solution, making them suitable for encapsulation or solubilization of hydrophobic or water-insoluble materials; and they also form bioerodible matrices for the sustained release of active agents.

Abstract: A liquid pharmaceutical composition is described comprising from about 7.5 mg/mL to about 12.5 mg/mL of midazolam in the form of midazolam maleate in solution in an aqueous liquid medium comprising ethanol and a polyhydroxy solvent. This composition can be administered by the buccal route for the treatment of patients suffering epileptic siezures or as an anaesthetic.

Abstract: Methods of reversing local anesthesia are disclosed. The methods comprise administering a local anesthetic and alpha adrenergic receptor agonist to induce local anesthesia followed by reversing anesthesia with a low dose of an alpha adrenergic receptor antagonist. Also disclosed are kits comprising a local anesthetic, an alpha adrenergic receptor agonist and a low dose of an alpha adrenergic receptor antagonist.

Abstract: The present invention is directed to medical devices or pharmaceutical composition, each containing a synthetic, biodegradable, biocompatible polymer that is the reaction product of a polybasic acid or derivative thereof, a monoglyceride, and a cationic polyol.

Abstract: The present invention describes food supplements that contain one or more fruit extracts useful for pain relief and anti-inflammation. The food supplements may be used to inhibit inflammation mediated by cyclooxygenase and more particularly by cyclooxygenase-2.

Abstract: A pharmaceutical composition for therapeutically treating prostate cancer, the pharmaceutical composition containing N-[6-methoxy-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-4-pyri midinyl]-2-phenylethenesulfoneamide or a pharmaceutically acceptable salt thereof as the effective component.

Abstract: Methods of reversing local anesthesia are disclosed. The methods comprise administering a local anesthetic and alpha adrenergic receptor agonist to induce local anesthesia followed by reversing anesthesia with a low dose of an alpha adrenergic receptor antagonist. Also disclosed are kits comprising a local anesthetic, an alpha adrenergic receptor agonist and a low dose of an alpha adrenergic receptor antagonist.

Abstract: The invention relates to surgical bone cement compositions and more particularly to bone cement compositions having aneasthetic properties, and to methods for producing analgesia.

Abstract: This invention relates to a pharmaceutical composition for oral administration comprising a carrier and, as active ingredient, an opioid (&mgr;receptor) agonist, such as fentanyl, or a salt thereof, characterized in that the composition is in the form of a fast-dispersing dosage form designed to release the active ingredient rapidly in the oral cavity. A process for preparing such a composition and the use of such a composition as an analgesic, for the treatment of chronic pain and/or breakthrough pain, as an anesthetic premedication, for the induction of anesthesia, as a sedative and/or for the treatment of anxiety are also provided.

Abstract: The present invention relates to an anesthetic composition containing a fluoroether compound and a physiologically acceptable Lewis acid inhibitor. This composition exhibits improved stability and does not readily degrade in the presence of a Lewis acid.

Abstract: The present invention relates to the use of xenon as a neuroprotectant and/or as an inhibitor of synaptic plasticity. In a preferred aspect, the xenon acts as an NMDA antagonist. The present invention also provides a method of reducing the level of activation of the NMDA receptors in a mammal, the method comprising modulating the activity of the NMDA receptor by administering to the mammal a therapeutically effective amount of xenon, wherein said reduction achieves neuroprotection and/or an inhibition of synaptic plasticity. A further embodiment of the invention provides a pharmaceutical composition for providing neuroprotection and/or inhibition of synaptic plasticity, together with a process for the preparation thereof.

Abstract: Melatonin (N-acetyl-5-methoxytryptamine), or its biologically active analogues, are used to induce anesthesia.

Abstract: A method for treating podotrochlosis (navicular disease/navicular syndrome) in the foot of a horse is disclosed. The method comprises identifying the specific area(s) of the horse's foot affected by navicular disease and applying at least one extracorporeal shockwave to the affected area(s). In a preferred embodiment, a sonar-emitting device is used to identify the areas within the foot affected by podotrochlosis.

Abstract: A pharmaceutical composition is described. The composition comprises a formulation. The formulation comprises an NMDA antagonist and an alpha-2 adrenergic agonist. In a preferred aspect, there is provided an improved anaesthetic comprising an NMDA antagonist and an alpha-2 adrenergic agonist.

Abstract: Melatonin (N-acetyl-5-methoxytryptamine), or its biologically active analogues, are used to induce anesthesia.

Abstract: An anesthetic is provided that includes a mixture of propofol, a tonicity agent, a substantially phospholipid-free emulsifying agent, a preservative such as benzyl alcohol, and water. This anesthetic is made by combining these components and then filtering the mixture of these components through a sterilizing filter. This anesthetic may be parenterally administered to both induce and maintain anesthesia in animals.

Abstract: The present invention relates to an anesthetic composition containing a fluoroether compound and a physiologically acceptable Lewis acid inhibitor. This composition exhibits improved stability and does not readily degrade in the presence of a Lewis acid.

Abstract: Methods of reversing local anesthesia are disclosed. The methods comprise administering a local anesthetic and alpha adrenergic receptor agonist to induce local anesthesia followed by reversing anesthesia with a low dose of an alpha adrenergic receptor antagonist. Also disclosed are kits comprising a local anesthetic, an alpha adrenergic receptor agonist and a low dose of an alpha adrenergic receptor antagonist.

Abstract: A sterile, stable pharmaceutical formulations of oil-in-water emulsions of Propofol containing no preservative are provided that comprise optimal amounts of egg lecithin and soybean oil, with a suitable pH range to prevent significant growth of microorganisms for at least 24 hours after adventitious, extrinsic contamination. The lower pH in the formulation has shown the most antimicrobial activity. The reduced amount of fat in the formulation also allows chronic sedation over extended periods of time with a reduced chance of fat overload in the blood.

Abstract: A polymethacrylate or other bone cement composition having analgesic properties is described. Bone cements containing up to 5% by weight of a local anaesthetic agent, such as lidocaine, have been demonstrated to elute sufficient lidocaine to provide an analgesic effect in vivo.

Abstract: Methods of treating glaucoma or elevated pressure and other diseases with reduced side effects by treating a mammal in need thereof an agonist of the alpha 2B or alpha 2B/2C adrenergic receptor(s). Also described are compounds having such selective agonist activity.

Abstract: The present invention is directed to a method for changing the body temperature of a patient by having them hyperventilate a gas mixture containing sulfur hexafluoride and oxygen. The method may be applied to cool patients in any clinical situation where induced hypothermia is desirable or to rapidly rewarm hypothermic patients. The invention also includes the gas mixtures used in the method.

Abstract: The present invention relates to an anesthetic composition containing a fluoroether compound and a physiologically acceptable Lewis acid inhibitor. This composition exhibits improved stability and does not readily degrade in the presence of a Lewis acid.

Abstract: The present invention relates to the use of xenon as an NMDA antagonist. In particular, the invention relates to a method of treatment comprising modulating the activity of an NMDA receptor in a mammal, the method comprising modulating the activity of the NMDA receptor by administering to the mammal a therapeutically effective amount of xenon. In a further aspect, the invention provides a process for the preparation of a pharmaceutical composition suitable for modulating the activity of an NMDA receptor.

Abstract: Extracts of Tanacetum parthenium with a reduced content of &agr;-unsaturated &ggr;-lactones, particularly of parthenolide, obtainable by elution on basic resins are disclosed. The extracts of the invention have favourable pharmacological properties together with reduced risks of allergic reactions.